荧光猝灭法测定替硝唑的含量

B-R缓冲溶液中,替硝唑可使十二烷基硫酸钠（SDS）的荧光猝灭,据此建立了荧光猝灭法测定替硝唑含量的方法.实验结果表明：在pH5～8缓冲溶液中,替硝唑浓度在0.2～5.0 mg·L^-1范围内与体系的荧光猝灭强度呈现良好的线性关系（R=0.998 4）,对浓度为0.2 mg·L^-1的替硝唑平行测定11次,检出限为6.4×10^-3mg·L^-1,RSD=1.91%,该法简便,快速,用于药物制剂中替硝唑含量的测定,结果满意.     

Determination of secnidazole in human plasma by high-performance liquid chromatography with UV detection and its application to the bioequivalence studies

A simple, accurate, precise and sensitive HPLC-UV method was developed for the determination of secnidazole in human plasma. Secnidazole and tinidazole (IS) were extracted from 0.2 mL of human plasma by ethyl acetate. Secnidazole was then separated by HPLC on a Diamond C(18) column and quantified by ultraviolet detection at 319 nm. The mobile phase consisted of acetonitrile-aqueous 5 mm sodium acetate (30:70, v/v) containing of 0.1% acetic acid adjusted to pH 4.0, and the flow rate was 1.0 mL/min. The low limit of quantification was 0.1 microg/mL. The method was linear over the concentration range 0.1-25.0 microg/mL (R(2) = 1.000). The recovery of secnidazole from human plasma ranged from 76.5 to 89.1%. Inter- and intra-assay precision ranged from 3.3 to 10.7%. Secnidazole in plasma was stable when stored at ambient temperature for 8 h, at -20 degrees C for 2 weeks and at -20 degrees C for three freeze-thaw cycles. The developed method was successfully applied to the pharmacokinetic and bioequivalence studies between test and reference secnidazole tablets following a single 500 mg oral dosage to 20 healthy volunteers of both genders. Pharmacokinetics parameters T(max), C(max), AUC(0-)t, AUC(0-infinity), T(1/2) were determined of both preparations. The analysis of variance (ANOVA) did not show any significant difference between the two preparations and 90% confidence intervals fell within the acceptable range for bioequivalence. It was concluded that the two secnidazole preparations are bioequivalence and may be used interchangeably.     

Crystal structures,thermal stabilities,and dissolution behaviours of tinidazole and the tinidazole–vanillic acid cocrystal: insights from energy frameworks

The crystal structures of the antimicrobial drug tinidazole [ TNZ ; systematic name: 1‐(2‐ethylsulfonylethyl)‐2‐methyl‐5‐nitroimidazole, C₈H₁₃N₃O₄S] and the 1:1 cocrystal of TNZ with the naturally occurring compound vanillic acid ( VA ; systematic name: 4‐hydroxy‐3‐methoxybenzoic acid, C₈H₈O₄), namely, the TNZ – VA cocrystal, were determined by single‐crystal X‐ray analysis at 100 K. The supramolecular structure of the TNZ – VA cocrystal is composed of a carboxylic acid dimer and an O—H…N(heterocycle) synthon in the form of layers made up of O—H…N and O—H…O hydrogen bonds. The layers are joined via C—H…O hydrogen bonds, π–π stacking and C—H…π interactions. The energy framework analysis, together with interaction energy calculations using the DLPNO‐CCSD(T) method, indicates that the TNZ – VA cocrystal inherits strong interactions from the TNZ and VA crystals, which accounts for the enhanced thermal stability and reduced dissolution rate. To the best of our knowledge, this is the first example of a cocrystal containing TNZ .     

母乳中甲硝唑、替硝唑测定及药代动力学

采用高效液相色谱法测定哺乳妇女单剂量静滴甲硝唑 ( 2 0mg/kg ,n =8)、替硝唑 ( 1 3mg/kg ,n =7)乳汁药物浓度 ,色谱柱为 pecoshereC1 8( 3μm ,3.3cm× 4.6mm) ,氯仿提取乳汁中药物 ,其平均回收率大于 88.8% .乳汁中甲硝唑与替硝唑药代动力学参数tmax,Cmax,t1 / 2Ke分别为 1 .7± 1 .0h ,2 0 .1 0± 4.95μg/mL ,6.4± 3.3h和 1 .3±0 .6h ,1 7.2 3± 3.1 2 μg/mL ,1 1 .0± 3.5h .     

Digitally enhanced thin layer chromatography for simultaneous determination of norfloxacin and tinidazole with the aid of Taguchi orthogonal array and desirability function approach: Greenness assessment by analytical Eco‐Scale

In this study, an eco‐friendly fast simple method was developed for simultaneous determination of norfloxacin and tinidazole based on thin‐layer chromatography and image‐processing analysis. The binary mixture was separated using reversed phase ‐ thin layer chromatography plates and 30% trifluoroacetic acid only as mobile phase. Mobile phase composition was optimized using Taguchi orthogonal array and Derringer's desirability function. The plates were viewed under UV lamp and photographed by iPhone camera followed by image processing with Fiji software using integrated density as the measured response. As decreasing illumination increases the sensitivity of the method, this method was applied on two different ranges for each drug. The first one was 0.6–6.0 and 0.9–9.0 µg/spot for norfloxacin and tinidazole, respectively measured on the original image with normal illumination. The second one was measured after decreasing the illumination of the captured images at 0.06–0.60 and 0.09–0.90 µg/spot for norfloxacin and tinidazole, respectively. The proposed method was successfully applied for the determination of both drugs in tablets dosage form without interference from the commonly encountered excipients. Analytical Eco‐Scale was used to evaluate the greenness profile of the proposed method and it was found to be excellent green analytical method.     

替硝唑-壳聚糖-海藻酸钠生物复合膜的缓释性能研究

系统研究了各种因素对复合膜的药物控释、稳定性、药物包埋率等性能的影响．最佳制备条件：pH=5．0、壳聚糖溶液质量分数为0．25％、海藻酸钠溶液质量分数为0．25％、海藻酸钠与壳聚糖的质量比为1：1．当壳聚糖溶液pH=5．0时,复合膜的药物控释性能最强．通过Ca^2＋的交联,使替硝唑的包埋率达到96．1％．复合膜的溶胀度研究表明,在pH=11的介质中具有最大的溶胀度．     

高效液相色谱法测定唾液中替硝唑浓度

用高效液相色谱法测定了唾液中替硝唑的浓度,以甲硝唑为内标,高氯酸沉淀蛋白后直接进样。方法简便、快速、回收率高、重现性好。     

盐酸左氧氟沙星与替硝唑联用对慢性盆腔炎的治疗效果评价

目的观察替硝唑联合盐酸左氧氟沙星治疗慢性盆腔炎的治疗效果。方法将天津河北区妇产科医院诊治的慢性盆腔炎患者随机分为研究组与对照组,对照组使用左氧氟沙星进行治疗,研究组替硝唑联合盐酸左氧氟沙星对患者进行治疗,对比两组的治疗效果与不良反应。结果经过治疗,研究组总有效率为93.3%,明显高于对照组83.3%(P0.05);研究组不良反应率5.0%低于对照组13.3%(P0.05)。结论替硝唑联合盐酸左氧氟沙星对于慢性盆腔炎患者来说,具有疗效好、安全性较高、不良反应较少等特点。